EP4227306A4 - HETEROCYCLIC SUBSTITUTED CONDENSED GAMMA-CARBOLINE DERIVATIVE, PROCESS THEREOF, INTERMEDIATE PRODUCT THEREOF AND USE THEREOF - Google Patents
HETEROCYCLIC SUBSTITUTED CONDENSED GAMMA-CARBOLINE DERIVATIVE, PROCESS THEREOF, INTERMEDIATE PRODUCT THEREOF AND USE THEREOF Download PDFInfo
- Publication number
- EP4227306A4 EP4227306A4 EP21876988.3A EP21876988A EP4227306A4 EP 4227306 A4 EP4227306 A4 EP 4227306A4 EP 21876988 A EP21876988 A EP 21876988A EP 4227306 A4 EP4227306 A4 EP 4227306A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- intermediate product
- heterocyclic substituted
- substituted condensed
- carboline derivative
- gamma
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- RDMFHRSPDKWERA-UHFFFAOYSA-N 5H-Pyrido[4,3-b]indole Chemical class C1=NC=C2C3=CC=CC=C3NC2=C1 RDMFHRSPDKWERA-UHFFFAOYSA-N 0.000 title 1
- 239000013067 intermediate product Substances 0.000 title 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/16—Peri-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Addiction (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011075840 | 2020-10-09 | ||
| CN202011074344 | 2020-10-09 | ||
| PCT/CN2021/122546 WO2022073470A1 (en) | 2020-10-09 | 2021-10-08 | HETEROCYCLIC SUBSTITUTED FUSED γ-CARBOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, INTERMEDIATE THEREOF AND USE THEREOF |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EP4227306A1 EP4227306A1 (en) | 2023-08-16 |
| EP4227306A4 true EP4227306A4 (en) | 2024-02-28 |
Family
ID=81125599
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP21876988.3A Pending EP4227306A4 (en) | 2020-10-09 | 2021-10-08 | HETEROCYCLIC SUBSTITUTED CONDENSED GAMMA-CARBOLINE DERIVATIVE, PROCESS THEREOF, INTERMEDIATE PRODUCT THEREOF AND USE THEREOF |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230339949A1 (en) |
| EP (1) | EP4227306A4 (en) |
| JP (1) | JP7561285B2 (en) |
| KR (1) | KR102894755B1 (en) |
| CN (1) | CN116568302B (en) |
| AU (1) | AU2021356875B2 (en) |
| BR (1) | BR112023005443A2 (en) |
| IL (1) | IL301847A (en) |
| MX (1) | MX2023004102A (en) |
| WO (1) | WO2022073470A1 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN120282964A (en) * | 2022-10-26 | 2025-07-08 | 上海枢境生物科技有限公司 | Mesylate and crystal form of heterocycle substituted condensed gamma-carboline derivative, and preparation method and application thereof |
| WO2025257090A1 (en) | 2024-06-10 | 2025-12-18 | Interquim, S.A. | Process for the preparation of synthesis intermediates of lumateperone and lumateperone analogues |
| WO2026011136A1 (en) * | 2024-07-03 | 2026-01-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2026011138A1 (en) * | 2024-07-03 | 2026-01-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000077002A1 (en) * | 1999-06-15 | 2000-12-21 | Du Pont Pharmaceuticals Company | Substituted heterocycle fused gamma-carbolines |
| US20170319580A1 (en) * | 2016-01-26 | 2017-11-09 | Intra-Cellular Therapies, Inc. | Organic compounds |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0905136A1 (en) * | 1997-09-08 | 1999-03-31 | Janssen Pharmaceutica N.V. | Tetrahydro gamma-carbolines |
| MXPA04001202A (en) | 2001-08-06 | 2005-02-17 | Pharmacia & Upjhon Company | Therapeutically useful tetracyclic ligands. |
| EP3085231A1 (en) * | 2008-05-27 | 2016-10-26 | Intra-Cellular Therapies, Inc. | Method and compositions for sleep disorders and other disorders |
| US8765760B2 (en) * | 2011-01-11 | 2014-07-01 | Sunovion Pharmaceuticals, Inc. | [1,2,4] triazol [1,5-a] pyrazines useful as inhibitors of phosphodiesterases |
| US10077267B2 (en) | 2014-04-04 | 2018-09-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2017117514A1 (en) * | 2015-12-31 | 2017-07-06 | Tung Roger D | Deuterated iti-007 |
| EP3525763B1 (en) * | 2016-10-12 | 2025-03-05 | Intra-Cellular Therapies, Inc. | Amorphous solid dispersions |
| RU2767410C2 (en) * | 2017-03-24 | 2022-03-17 | Интра-Селлулар Терапиз, Инк. | New compositions and methods |
-
2021
- 2021-10-08 MX MX2023004102A patent/MX2023004102A/en unknown
- 2021-10-08 KR KR1020237009354A patent/KR102894755B1/en active Active
- 2021-10-08 CN CN202180068356.7A patent/CN116568302B/en active Active
- 2021-10-08 EP EP21876988.3A patent/EP4227306A4/en active Pending
- 2021-10-08 WO PCT/CN2021/122546 patent/WO2022073470A1/en not_active Ceased
- 2021-10-08 BR BR112023005443A patent/BR112023005443A2/en unknown
- 2021-10-08 JP JP2023546376A patent/JP7561285B2/en active Active
- 2021-10-08 US US18/027,226 patent/US20230339949A1/en active Pending
- 2021-10-08 IL IL301847A patent/IL301847A/en unknown
- 2021-10-08 AU AU2021356875A patent/AU2021356875B2/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000077002A1 (en) * | 1999-06-15 | 2000-12-21 | Du Pont Pharmaceuticals Company | Substituted heterocycle fused gamma-carbolines |
| US20170319580A1 (en) * | 2016-01-26 | 2017-11-09 | Intra-Cellular Therapies, Inc. | Organic compounds |
Non-Patent Citations (1)
| Title |
|---|
| See also references of WO2022073470A1 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2021356875B2 (en) | 2023-11-23 |
| KR20230054417A (en) | 2023-04-24 |
| US20230339949A1 (en) | 2023-10-26 |
| KR102894755B1 (en) | 2025-12-02 |
| MX2023004102A (en) | 2023-04-27 |
| BR112023005443A2 (en) | 2023-05-09 |
| JP7561285B2 (en) | 2024-10-03 |
| WO2022073470A1 (en) | 2022-04-14 |
| CA3194682A1 (en) | 2022-04-14 |
| EP4227306A1 (en) | 2023-08-16 |
| IL301847A (en) | 2023-06-01 |
| AU2021356875A1 (en) | 2023-05-25 |
| JP2023544653A (en) | 2023-10-24 |
| CN116568302B (en) | 2025-04-18 |
| AU2021356875A9 (en) | 2024-02-08 |
| CN116568302A (en) | 2023-08-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE INTERNATIONAL PUBLICATION HAS BEEN MADE |
|
| PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
| STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: REQUEST FOR EXAMINATION WAS MADE |
|
| 17P | Request for examination filed |
Effective date: 20230405 |
|
| AK | Designated contracting states |
Kind code of ref document: A1 Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR |
|
| DAV | Request for validation of the european patent (deleted) | ||
| DAX | Request for extension of the european patent (deleted) | ||
| A4 | Supplementary search report drawn up and despatched |
Effective date: 20240129 |
|
| RIC1 | Information provided on ipc code assigned before grant |
Ipc: A61P 25/30 20060101ALI20240123BHEP Ipc: A61P 25/28 20060101ALI20240123BHEP Ipc: A61P 25/24 20060101ALI20240123BHEP Ipc: A61P 25/22 20060101ALI20240123BHEP Ipc: A61P 25/20 20060101ALI20240123BHEP Ipc: A61P 25/14 20060101ALI20240123BHEP Ipc: A61P 25/18 20060101ALI20240123BHEP Ipc: A61P 25/00 20060101ALI20240123BHEP Ipc: A61K 31/4985 20060101ALI20240123BHEP Ipc: C07D 471/16 20060101AFI20240123BHEP |